Hour, Mann-Jen; Huang, Li-Jiau; Kuo, Sheng-Chu; Xia, Yi; Bastow, Kenneth; Nakanishi, Yuka; Hamel, Ernest; Lee, Kuo-Hsiung published the artcile< 6-Alkylamino- and 2,3-Dihydro-3'-methoxy-2-phenyl-4-quinazolinones and Related Compounds: Their Synthesis, Cytotoxicity, and Inhibition of Tubulin Polymerization>, Quality Control of 5004-88-6, the main research area is quinazolinone dihydroquinazolinone preparation cytotoxicity tubulin polymerization inhibition; antitumor activity quinazolinone dihydroquinazolinone; antimitotic potential quinazolinone dihydroquinazolinone.
As part of the authors’ continuing search for potential anticancer candidates among 2-phenyl-4-quinolones and 2-phenyl-4-quinazolinones, two series of 6,7,2′,3′,4′,5′-substituted 2-phenyl-4-quinazolinones (shown as I) and 6,2′,3′,4′,5′-substituted 2,3-dihydro-2-phenyl-4-quinazolinones (shown as II) were synthesized and evaluated for cytotoxicity and as inhibitors of tubulin polymerization In general, a good correlation was found between the two activities. Five of the 6-substituted heterocyclic 2-phenyl-4-quinazolinones showed significant cytotoxicity against a panel of human tumor cell lines with EC50 values in the low micromolar to nanomolar concentration ranges. Compound 38 (I; R6 = pyrrolino; R7 = R2′ = R4′ = R5′ = H; R3′ = OMe) was the most potent of these compounds, as well as the most potent inhibitor of tubulin polymerization in this series. The activity of 38 was in the same range as those of the antimitotic natural products, colchicine, podophyllotoxin, and combretastatin A-4. Substituted 2-phenyl-4-quinazolinones and 2,3-dihydro-2-phenyl-4-quinazolinones also displayed highly selective cytotoxicity against the ovarian cancer 1A9 and P-gp resistant KB-VIN cell lines.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Quality Control of 5004-88-6.
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